Two novel Mg(II)-based and Zn(II)-based complexes: inhibiting growth of human liver cancer cells

Two new Mg(II)-based and Zn(II)-based coordination polymers, {[Mg3(BTB)(DMA)4](DMA)2}n (1, H3BTB=1,3,5-benzenetrisbenzoic acid, DMA=N,N-dimethylacetamide) and {(H2NMe2)2[Zn3(BTB)2(OH)(Im)](DMF)9(MeOH)7}n (2, Im=imidazole, DMF=N,N-dimethylformamide), have been successfully synthesized and structurally characterized under solvothermal conditions. 1 contains a linear [Mg3(COO)6] cluster that connected by the fully deprotonated BTB3- ligands to give a kgd-type 2D bilayer structure; 2 represents a microporous 3D pillar-layered system based on the binuclear Zn units and pillared Im ligands, which shows a (3,5)-connected hms topological net. In addition, in vitro anticancer activities of compounds 1 and 2 on 4 human liver cancer cells (HB611, HHCC, BEL-7405 and SMMC-7721) were determined.

Synthesis and evaluation of coumarin derivatives against human lung cancer cell lines

Series of novel coumarin derivatives [I (a-d) and II (a-d)] were successfully synthesized and their structures were determined based on infrared 1H-nuclear magnetic resonance (NMR), HRMS, and single crystal X-ray crystallography. Additionally, the new synthesized compounds were evaluated to identify the molecular characteristics that contribute to their cytotoxicity, which was tested against SK-LU-1, SPC-A-1 and 95D human lung cancer cell lines, using the MTT assay. The results of this study showed that compounds Ic, Id, IIc, and IId exhibited an efficient percentage of inhibition of cell proliferation.

Children's eating behavior: comparison between normal and overweight children from a school in Pelotas, Rio Grande do Sul, Brazil / Comportamento alimentar infantil: comparação entre crianças sem e com excesso de peso em uma escola do município de Pelotas, RS

OBJECTIVE: To evaluate differences in children's eating behavior in relation to their nutritional status, gender and age. METHODS: Male and female children aged six to ten years were included. They were recruited from a private school in the city of Pelotas, Rio Grande do Sul, southern Brazil, in 2012. Children´s Eating Behaviour Questionnaire (CEBQ) subscales were used to assess eating behaviors: Food Responsiveness (FR), Enjoyment of Food (EF), Desire to Drink (DD), Emotional Overeating (EOE), Emotional Undereating (EUE), Satiety Responsiveness (SR), Food Fussiness (FF) and Slowness in Eating (SE). Age-adjusted body mass index (BMI) z-scores were calculated according to the WHO recommendations to assess nutritional status. RESULTS: The study sample comprised 335 children aged 87.9±10.4 months and 49.3% had normal weight (n=163), 26% were overweight (n=86), 15% were obese (n=50) and 9.7% were severely obese (n=32). Children with excess weight showed higher scores at the CEBQ subscales associated with "food approach" (FR, EF, DD, EOE, p<0.001) and lower scores on two "food avoidance" subscales (SR and SE, p<0.001 and p=0.003, respectively) compared to normal weight children. Differences in the eating behavior related to gender and age were not found. CONCLUSIONS: "Food approach" subscales were positively associated to excess weight in children, but no associations with gender and age were found. .

OBJETIVO: Avaliar diferenças no comportamento alimentar infantil em função do estado nutricional, do sexo e da idade. MÉTODOS: O estudo incluiu crianças na faixa de seis a dez anos, de ambos os sexos, de uma escola privada em Pelotas (RS), em 2012. Para avaliar o comportamento alimentar usaram-se as subescalas do questionário Children's Eating Behaviour Questionnaire (CEBQ): resposta à comida (FR), prazer de comer (EF), desejo de beber (DD), sobreingestão emocional (EOE), subingestão emocional (EUE), resposta à saciedade (SR), seletividade (FF) e ingestão lenta (SE). Avaliou-se o estado nutricional por meio do escore-z do IMC/idade. RESULTADOS: Participaram 335 crianças de 87,9±10,4 meses. Apresentaram eutrofia 49,3% (n=163), sobrepeso 26% (n=86), obesidade 15% (n=50) e obesidade grave 9,7% (n=32). Crianças com excesso de peso tiveram maior pontuação nas subescalas de "interesse pela comida" (FR, EF, DD, EOE, p<0,001) e menor pontuação nas subescalas de "desinteresse pela comida" (SR e SE, p<0,001 e p=0,003, respectivamente), se comparadas com as crianças com peso adequado. Não foram observadas diferenças no comportamento alimentar segundo sexo e idade. CONCLUSÕES: Observou-se que comportamentos alimentares que refletem "interesse pela comida" estão associados positivamente ao excesso de peso, mas não foi encontrada associação com o sexo e a idade da criança. .

Factors impacting the growth and nutritional status of cystic fibrosis patients younger than 10 years of age who did not undergo neonatal screening / Fatores que afetam o crescimento e estado nutricional de pacientes com fibrose cística com idade inferior a 10 anos e que não foram submetidos à triagem neonatal

OBJECTIVE: The aim of this study was to evaluate by clinical and laboratory parameters how cystic fibrosis (CF) affects growth and nutritional status of children who were undergoing CF treatment but did not receive newborn screening. METHODS: A historical cohort study of 52 CF patients younger than 10 years of age were followed in a reference center in Campinas, Southeast Brazil. Anthropometric measurements were abstracted from medical records until March/2010, when neonatal screening program was implemented. Between September/2009 and March/2010, parental height of the 52 CF patients were also measured. RESULTS: Regarding nutritional status, four patients had Z-scores ≤-2 for height/age (H/A) and body mass index/age (BMI/A). The following variables were associated with improved H/A ratio: fewer hospitalizations, longer time from first appointment to diagnosis, longer time from birth to diagnosis and later onset of respiratory disease. Forced vital capacity [FVC(%)], forced expiratory flow between 25-75% of FVC [FEF25-75(%)], forced expiratory volume in the first second [FEV1(%)], gestational age, birth weight and early respiratory symptoms were associated with improved BMI/A. CONCLUSIONS: Greater number of hospitalizations, diagnosis delay and early onset of respiratory disease had a negative impact on growth. Lower spirometric values, lower gestational age, lower birth weight, and early onset of respiratory symptoms had negative impact on nutritional status. Malnutrition was observed in 7.7% of cases, but 23% of children had nutritional risk. .

OBJETIVO: Avaliar por meio de parâmetros clínicos e laboratoriais como a fibrose cística (FC) afeta o crescimento e estado nutricional de crianças submetidas ao tratamento de FC que não foram submetidas à triagem neonatal. MÉTODOS: Uma coorte histórica com 52 pacientes com FC menores de 10 anos foi acompanhada em um centro de referência em Campinas, Sudeste do Brasil. Peso e altura foram coletados de prontuários médicos até março de 2010, quando a triagem neonatal foi implementada. Entre setembro de 2009 a março de 2010 a altura dos pais foi medida. RESULTADOS: Quatro pacientes tiveram escores Z ≤ -2 para altura/idade (A/I) e índice de massa corporal/idade (IMC/A). As seguintes variáveis foram associadas com melhor razão A/I: menor número de hospitalizações, maior tempo entre a primeira consulta e o diagnóstico, maior tempo entre o nascimento e o diagnóstico e início tardio da doença respiratória. Capacidade vital forçada [CVF(%)], fluxo expiratório forçado entre 25-75% da CVF [FEF25-75(%)], volume expiratório forçado no primeiro segundo [VEF1(%)], idade gestacional, peso ao nascer e início dos sintomas respiratórios foram associados com melhor IMC/I. CONCLUSÕES: Maior número de hospitalizações, retardo no diagnóstico e início precoce da doença respiratória tiveram impacto negativo no crescimento. Menores valores espirométricos, menor idade gestacional, menor peso ao nascer e o início precoce dos sintomas respiratórios tiveram impacto negativo no estado nutricional. A desnutrição foi observada em 7,7% dos casos, mas 23% das crianças apresentaram risco nutricional. .

Vitamin D deficiency in pregnancy and its impact on the fetus, the newborn and in childhood / Deficiência de vitamina D na gravidez e o seu impacto sobre o feto, o recém-nascido e na infância

OBJECTIVE: Vitamin D deficiency (VDD) in pregnant women and their children is an important health problem with severe consequences for the health of both. Thus, the objectives of this review were to reassess the magnitude and consequences of VDD during pregnancy, lactation and infancy, associated risk factors, prevention methods, and to explore epigenetic mechanisms in early fetal life capable of explaining many of the non-skeletal benefits of vitamin D (ViD). DATA SOURCE: Original and review articles, and consensus documents with elevated level of evidence for VDD-related clinical decisions on the health of pregnant women and their children, as well as articles on the influence of ViD on epigenetic mechanisms of fetal programming of chronic diseases in adulthood were selected among articles published on PubMed over the last 20 years, using the search term VitD status, in combination with Pregnancy, Offspring health, Child outcomes, and Programming. DATA SYNTHESIS: The following items were analyzed: ViD physiology and metabolism, risk factors for VDD and implications in pregnancy, lactation and infancy, concentration cutoff to define VDD, the variability of methods for VDD detection, recommendations on ViD replacement in pregnant women, the newborn and the child, and the epigenetic influence of ViD. CONCLUSIONS: VDD is a common condition among high-risk pregnant women and their children. The routine monitoring of serum 25(OH)D3 levels in antenatal period is mandatory. Early preventive measures should be taken at the slightest suspicion of VDD in pregnant women, to reduce morbidity during pregnancy and lactation, as well as its subsequent impact on the fetus, the newborn and the child. .

OBJETIVO: Deficiência de vitamina D (DVD) nas gestantes e seus filhos é problema de saúde, com consequências graves à saúde de ambos. Assim, esta revisão visou reavaliar a magnitude e as consequências da DVD na gestação, lactação e infância, fatores de risco associados, métodos de prevenção, além de explorar os mecanismos epigenéticos na vida fetal capazes de explicar benefícios não-esqueléticos da vitamina D (ViD). FONTES DE DADOS: Selecionaram-se artigos originais, de revisão e consensos com nível elevado de evidência para decisões clínicas relacionadas à DVD na saúde das gestantes e seus filhos e artigos sobre sua ação sobre os mecanismos epigenéticos da programação fetal de doenças crônicas na vida adulta, publicados no PubMed nos últimos 20 anos, empregando-se VitD status, e em combinação com Pregnancy, Offspring health, Child outcomes e Programming. SÍNTESE DOS DADOS: Abordou-se fisiologia, metabolismo, fatores de risco para a DVD e implicações na gravidez, lactação e infância, concentração de corte para definir DVD, variabilidade de métodos na sua detecção, recomendações sobre a reposição de ViD nas gestantes, no recém-nascido e na criança, bem como sobre ter as influências epigenéticas da ViD. CONCLUSÕES: DVD é frequente entre gestantes de alto risco e seus filhos. Monitorar rotineiramente os níveis séricos de 25(OH)D3 no período antenatal é imperativo. Medidas preventivas precoces devem ser instituídas à menor suspeita de DVD na gestante, para reduzir morbidades durante a gestação e a lactação, bem como seu posterior impacto sobre o feto, o recém-nascido e na infância. .

Neuropsychomotor developmental delay: conceptual map, term definitions, uses and limitations / Atraso do desenvolvimento neuropsicomotor: mapa conceitual, definições, usos e limitações do termo

OBJECTIVE: To retrieve the origin of the term neuropsychomotor developmental delay" (NPMD), its conceptual evolution over time, and to build a conceptual map based on literature review. DATA SOURCE: A literature search was performed in the SciELO Brazil, Web of Science, Science Direct, OneFile (GALE), Pubmed (Medline), Whiley Online, and Springer databases, from January of 1940 to January of 2013, using the following keywords: NPMD delay, NPMD retardation, developmental delay, and global developmental delay. A total of 71 articles were selected, which were used to build the conceptual map of the term. DATA SYNTHESIS: Of the 71 references, 55 were international and 16 national. The terms developmental delay and global developmental delay were the most frequently used in the international literature and, in Brazil, delayed NPMD was the most often used. The term developmental delay emerged in the mid 1940s, gaining momentum in the 1990s. In Brazil, the term delayed NPMD started to be used in the 1980s, and has been frequently cited and published in the literature. Delayed development was a characteristic of 13 morbidities described in 23 references. Regarding the type of use, 19 references were found, with seven forms of use. Among the references, 34 had definitions of the term, and 16 different concepts were identified. CONCLUSIONS: Developmental delay is addressed in the international and national literature under different names, various applications, and heterogeneous concepts. Internationally, ways to improve communication between professionals have been indicated, with standardized definition of the term and use in very specific situations up to the fifth year of life, which was not found in Brazilian publications. .

OBJETIVO: Resgatar a origem do termo atraso do desenvolvimento neuropsicomotor (DNPM), sua evolução conceitual ao longo do tempo e construir mapa conceitual do termo com base em busca bibliográfica. FONTES DE DADOS: Foi realizada busca nas bases de dados eletrônicas do Portal da Capes, que incluem Scielo Brazil, Web of Science, Science Direct, OneFile (GALE), Pubmed (Medline), Whiley Online e Springer, referente a Janeiro/1940-Janeiro/2013. Palavras-chave: atraso e retardo do DNPM, developmental delay e global developmental delay. Foram selecionados 71 artigos e construído o mapa conceitual do termo. SÍNTESE DE DADOS: Das 71 referências, 55 eram internacionais e 16 nacionais. Os termos mais encontrados foram global developmental delay e developmental delay na literatura internacional e retardo e atraso do DNPM no Brasil. Internacionalmente, o termo surgiu em meados da década de 40 ganhando força nos anos 90. No Brasil, o termo começou a ser usado na década de 80 e vem sendo frequentemente citado na literatura. O atraso é citado em 23 trabalhos como característica presente em 13 tipos de condições clínicas. Com relação ao uso, foram encontrados 19 estudos, com sete situações de uso. Dentre os artigos revisados, 34 deles apresentaram definições, sendo identificados 16 conceitos diferentes. CONCLUSÕES: O atraso do desenvolvimento é abordado na literatura internacional e nacional sob diversos nomes, diferentes aplicações e conceitos heterogêneos. Internacionalmente, apontam-se caminhos para melhorar a comunicação entre profissionais, com definição padronizada do termo e uso em situações específicas até o quinto ano de vida, o que não foi encontrado nas publicações nacionais. .

Síntesis y evaluación preliminar de la posible actividad antimalárica y antineoplásica de derivados 7-cloroquinolina-4-sustituidos / Synthesis and preliminary evaluation of antimalarial and antineoplastic possible activity of 7-chloroquinoline-4-substituted derivatives

En el presente trabajo se describe la síntesis y la evaluación de la posible actividad Antimalárica y Antineoplásica de una serie de derivados 7-cloroquinolina-4-sustituidos. La estrategia empleada para la síntesis comienza con las obtención de los intermediarios clave 1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)etanona (2 y 3) mediante una sustitución nucleofílica aromática entre la 4,7-dicloroquinolina y la 3 y/o 4-amino acetofenona. Los derivados (E)-1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)-3-(fenilsustituido)prop-2-eno-1-ona (4 y 5), se sintetizaron a través de una condensación aldólica de Claisen-Schmidt entre los intermediarios clave y diferentes benzaldehídos sustituidos. Los derivados 7-cloro-N-(3 ó 4-(4,5-dihidro-5-(fenilsustituido)-1H-pirazol-3-il)fenil)quinolin-4-amina (6 y 7) y los 1-(3 ó 4-(7-cloroquinolin-4-ilamino)fenil)-3-(fenilsustituido)propano-1-ona (8 y 9) se diseñaron por modificación molecular de la cetona a,b-insaturada de los compuestos finales 4 y 5, (metodología clásica de la Química Medicinal) para obtener dichos derivados rígidos 6 y 7, mediante la formación de un anillo D2-pirazolina y flexibles 8 y 9, a través de su reducción. La síntesis de los derivados 6 y 7 se realizó mediante una reacción de ciclo-condensación con hidrazina monohidratada y los derivados 8 y 9, se obtuvieron a través de una hidrogenación catalítica. En la evaluación de la actividad Antimalárica in vitro se evidenció que los derivados 4, 5, 6 y 7, mostraron actividades inhibitorias la formación de la b hematina importantes (superior al 70 %), siendo los más activos: 4l, 5g, 5c, 5g y 6e, 6f con valores comparable al de la CQ. En la evaluación Antimalárica in vivo se encontró que el derivado 4e fue el más activo con 26,4 días de sobrevivencia post-infección (230 % de incremento) y una parasitemia de 2,4 % (96 % de reducción). Con respecto a los resultados obtenidos en el efecto de estos derivados sobre la viabilidad y proliferación de las líneas celulares neoplásicas Jurkat E6.1, HL60, MCF-7 y A549, los compuestos 4a, 4g, 4l, 4m y 6e mostraron la mayor actividad inhibitoria del crecimiento de las células leucémicas HL60 después de 24h de tratamiento con valores de CI50 de 1,19 µM, 1,08 µM, 0,59 µM, 0,43 µM y 0,94 µM (hasta 3 y 100 veces más activos que la doxorubicina y que la CQ, respectivamente). En lo referente a la evaluación de la actividad proapoptótica en las líneas celulares neoplásicas Jurkat E6.1, HL60, MCF-7 y A549, se evidenció que los derivados 4, 5 y 6, al igual que los controles, generaron un aumento en el porcentaje de células positivas para la Anexina V/FITC dependiente de la dosis (apoptosis temprana y tardía). Ninguno de estos derivados indujo el proceso de necrosis en estas células.

The present investigation describes the synthesis and evaluation of the Antimalarial and Antineoplastic activity possible a series of derivatives of 7-substituted-4-chloro-quinoline. The strategy employed for the synthesis begins with preparation of the key intermediate 1-(3 or 4-(7-chloroquinolin-4-ylamino) phenyl)ethanone (2and 3) by a nucleophilic aromatic substitution between 4,7-dichloroquinoline and the 3 and/or4-amino acetophenone. The derivatives (E)-1-(3 or 4-(7-chloroquinolin-4-ylamino) phenyl)-3-(substitutedphenyl)prop-2-en-1-one (4and 5), were synthesized a through aldol condensation Claisen-Schmidt among different key intermediates and substituted benzaldehydes. The resulting 7-chloro-N-(3 or 4-(4,5-dihydro-5-(substitutedphenyl)-1H-pyrazol-3-yl)phenyl)quinolin-4-amine (6 and 7) and 7-chloro-4-[(3 or 4-(substituted phenyl)ethylcarbonyl)phenyl]aminoquinoline(8 and 9) were designed for the molecular modification , -unsaturated ketone of the final compounds 4and 5 (classic methodology Medicinal Chemistry) for said rigid derivatives 6and 7, through the formation of a 2-pyrazoline ring flexible and 8and 9, through its reduction. The synthesis of derivatives 6and 7were performed using a cycle-condensation reaction with hydrazine monohydrate and 8and 9derivatives were obtained via a catalytic hydrogenation. In the assessment of antimalarial activity in vitro was demonstrated that derivatives 4, 5, 6and 7showed inhibitory activities forming the major hematin (above 70%), being more active: 4l, 5g, 5c, 5g, 6eand 6f,with values comparable to that of CQ. In vivoantimalarial evaluation found that the derivative 4ewas most active with survival 26.4 dayspost-infection (230% increase) and a parasitemia of 2.4% (96% reduction). With regard to the results on the effect of these derivatives on the viability and proliferation of neoplastic cell lines Jurkat E6.1, HL60, MCF-7 and A549, compounds 4a, 4g, 4l,4mand 6eshow greater activity growth inhibitory HL60 leukemia cells after 24 h of treatment with IC50values of 1.19µM, 1.08µM, 0.59µM, 0.43µMand 0.94 M (to 3 and 100 times more active than doxorubicin and the CQ, respectively). Regarding the evaluation of pro-apoptotic activity on neoplastic cell lines Jurkat E6.1, HL60, MCF-7 and A549, was demonstrated that derivatives 4, 5and 6, like the controls, an increase in generated percentage of cells positive for Annexin V/FITC dose dependent (early andlate apoptosis). None of these derivatives induced necrosis process in these cells.

Design and synthesis of new EGFR- tyrosine kinase inhibitors containing pyrazolo[3,4-pywmidine cores as anticancer agents

New designed EGFR inhibitors [7-1 1] were prepare dfrom the pyrazolo[3t4-d]pyrimidine intermediates 4a-d including different moieties. All newly synthesized compounds were confirmed by elemental analyses and spectral data. The molecular simulation docking to protein tyrosine kinase [EGFR], using erlotinib [Tarceva[TM]] as a lead compound was also studied. Some of the prepared compounds were screened for in-vitro cytotoxic activity. The docking results were in coincidence with the biological results that indicated compound 7a showed an inhibitory activity against human breast carcinoma cell line [MCF-7] [1C so [14.86microM]

Flavonoid glycosides of myriophyllum spicatum and cytotoxic activity

Eight flavonoid compounds were isolated and identified for first time from the aquatic plant myriophyllum spicatuin. Their structural were established on the basis of detailed chemical and spectral analysis. The cytotoxic activity of the plant extracts against liver, brain and breast human cell lines were evaluated

Molecular mechanics aided design of antineoplastic agents from ruthenium coordinate complexes.

Through energy minimization using molecular mechanics force field four ruthenium cordinate complexes have been synthesized. Compound I to IV showed antineoplastic activity with varying degree on EAC bearing mice. Mode of action may be through inhibition of antioxidant property of tumor cell as evident from lipid peroxidase activity. Among the complexes Bis pyridine tetrachloro ruthenium exhibits highest order of activity with respect to increase mean survival time, inhibition of tumour volume, total blood count, hemoglobin and lipid peroxidase activity.

Síntese e atividade biológica de novas tiossemicarbazonas / Synthesis and biological activity of new thiosemicarbazones

Este trabalho descreve a síntese e avaliaçäo estrutural de nove tiossemicarbazonas, obtidas pela condensaçäo de ariltioacetaldeídos e artiopropanonas substituídas com cloridrato de tiossemicarbazida. Estes novos compostos foram testados in vitro pelo fitoteste Lepidium sativum. Todos eles apresentaram atividade inibidora do crescimento celular (pI50) superior àquela de 5-fluoruacila, composto anticancerígeno, utilizado como referência.

Synthesis of some new pyrimidine derivatives as potential anticancer and anti-HIV agent.

Several 2,4-diaminopyrimidines have been synthesized and tested for their anticancer and anti-HIV activities. Out of these, eight compounds displayed significant activity against leukemia, melanoma, non-small cell and CNS cancer. Two compounds were active against leukemia P388. One compound has been found to be moderately active as compared to AZT.

Synthesis and antitumor activity of certain thienopyridine and pyridothienopyrimidine derivatives

A series of cyclopenteno[b] or tetrahydrobenzo[b]thiophenes, tetrahydrothieno[2,3-c]pyridines and tetrahydropyrido[4',3' :4,5]thieno[2,3-d]pyrimidines was synthesized as antitumor agents. Most of the tested compounds showed cytotoxic effect [GI[50] < 10 [micro]M] against the growth of P388 leukemia cells. Ethyl2-phenylsulphonamido-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxylate [lla], Ethyl 2-[4- bromo-phenylsulphonamido]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxylate [llb], Ethyl 2-[4-methylphenyl-sulphonamido]-4,5,6,7-tetrahydrobenzo[b]thiophen-3-carboxylate [IIc], Ethyl 2-[4-methoxybenzamido]-4,5,6,7 -tetrahydro[b]thiophen-3-carboxylate [IIIc] and N-[4-methylphenyl] N-[3-carbo-ethoxy-6-methyl-4,5,6,7-tetrahydrothieno[2,3-c] pyridin-2-yl] thiourea [lVc] showed strong potency [GI [50]; 0.8, 1.15,2.09, 1.3,2.25 [micro]M; respectively]. The detailed synthesis, spectroscopic and biological data are reported

Synthesis and antitumor activity of some 9- [4-substituted sulfamoylphenylamino] acridine-4-hydroxyalkylcarboxamide derivatives: Part II1

A series of 9-[4-substituted sulfamoylphenyl-amino] acridine-4-hydyroxyalkyl carboxamide derivatives has been synthesized in order to study the SAR of this class of compounds. The prepared final compounds have been evaluated for antitumor activity in NIH, Bethesda, Maryland, USA. No significant activity has been observed

Synthesis of certain substituted quinolines as potential DNA complexing agents

Two series of 2,4,6-trisubstituted quinoline derivatives were prepared for potential DNA complexing activity. The first series comprises the preparation of 4-arylaminoquinoline derivatives 9-24 by amination of 4-chloroquinolines 5-8, while, the second series involves the preparation of the amide derivatives of cinchoninic acid 27-30 by amidation of 2-phenyl-4-cinchonoyl chloride 26. Three new compounds were tested for in vitor cytotoxic activity

1-arylcycloalkyl [bis [2-chloromethyl]] amines: alkylating analogs of PCP as possible antineoplastic agents for brain tumors

Novel alkylating analogs of phencyclidine [PCP] have been synthesized in the hope of targeting brain tumors. The compounds were designed to fulfill the skeletal requirements of PCP and those of nitrogen mustard analogs. Chemically, the new compounds would be considered as 1-arylcycloalkyl [bis [2-chloroethyl]] amines

Synthesis of some substituted 9-anilinoacridines and 4-anilinoquinolines of possible antitumor activity

3-amino-4-methoxybenzoie acid methyl ester and 3-amino- 4-methoxy-6- methane sulphonamidobenzoic acid methyl ester were condensed with 4, 7-dichloroquinoline, 4-chloroquinaldine, 9-chloroacridine and 2-methoxy-6,9-dichloro acridine. The anilide esters obtained were reduced to the corresponding alcohols from which the N-methylcarbamate derivatives were prepared as possible antitumour agents

Pynido [223-of] pyrimiduies: deaza-analges of pteriduies as possible anti neoplastic agents

A novel series of 4-amino-2-thioxo [or substituted thio]pyrido [2, 3-d] pyrimidines IX-XXIV, and 2,4-dithioxo [or dialkylthio] pyrido [2, 3-d] pyrimidines XXV-XXX was synthesized as possible antineoplastic agents. The versatile synthetic approach involved cycloaddition of 2-[3-benzoylthioureido] function on the 3-cyano moiety in the pyridine derivatives VI-VIII. Some of the newly synthesized compounds were subjected to preliminary biological evaluation involving in vitro disease-oriented antitumor screen as well as anti-AIDS drug discovery program against HIV. None of the selected compounds showed any significant activity

N1, N3-diarly sulfonylureas as possible anticancer agents

This study described the synthesis of a number of sulofenur thiadiazole analogues with structural modification of the aryl moiety of the sulfonamide portion of the diaryl sulfonylureas. Two different methods were adopted in order to prepare the target compounds. The new compounds were evaluated for in vitro cytotoxic activity. Two compounds showed 100% activity against Ehrlich ascites tumor cells